Course Catalog

Drug-like Properties: Optimizing Pharmacokinetics and Safety in Drug Discovery

This course increases your practical knowledge of pharmacokinetics and toxicity and proven approaches to optimize compounds for drug discovery success; gain knowledge on crucial drug-like properties, useful structure modification strategies, SAR, and lead selection and optimization.

Course Details

Key Topics

  • Essentials of drug properties and practical real-world applications.
  • Pharmacokinetics from a non-mathematical, practical viewpoint.
  • Understand and apply PK clearance, half-life, volume of distribution, bioavailability, AUC, Cmax.
  • How drug properties (physicochemical, metabolic, transporter) affect absorption, distribution, metabolism and excretion (ADME) and PK of drugs.
  • Successful structure modification strategies to improve drug properties and pharmacokinetics.
  • Case examples on optimizing drug properties, pharmacokinetics and safety.
  • Effects of compound properties on discovery pharmacology (in vitro, in vivo pharmacology, PK).
  • In silico, in vitro and in vivo methods for assessing drug properties.

Information

Drug metabolism, pharmacokinetics (PK) and toxicity are critical components of successful drug discovery research. This course provides a practical working knowledge of PK and toxicity. Properties that affect PK and toxicity are discussed (i.e., physicochemical, metabolic, transporter, toxic). Proven strategies for structure modification to improve property performance and structure-property relationships are described. Numerous cases examples from the literature illustrate successful lead selection and optimization. Property assays are discussed to assist informed decisions and interpretation of the data.

Registrants are encouraged to purchase the book, Drug-Like Properties: Concepts, Structure Design and Methods: From ADME to Toxicology, in addition to their registration as part of this course. To purchase this book at a discount through ACS, please contact Andrea Adams. Quantities are limited.

Who Should Attend

Medicinal chemists and other discovery scientists who design, synthesize, and test new drug candidates, lead research teams, or measure and predict ADMET properties of compounds. Registrants should possess a basic knowledge of drug discovery.

Benefits

  • Understand each property and how they affect your success.
  • Gain practical knowledge of pharmacokinetics and toxicity.
  • Develop confidence with interpreting pharmacokinetics parameters and correlations to in vivo pharmacodynamics.
  • Apply drug property data to hit selection, lead optimization, and clinical candidate selection.
  • Become familiar with ADMET property assays for more informed data interpretation.
  • Practice property concepts by participating in individual and group real-world exercises.
  • Learn about case studies in which leads were successfully optimized to improve candidate quality.
  • Diagnose the properties causing poor pharmacokinetics.
  • Learn approaches to improve compound series.

Agenda

  • The Importance of Pharmaceutical Properties – why quality drug properties are necessary for discovering successful clinical candidates
  • Comprehensive Survey of Drug Properties that are Crucial for Discovery – Practical fundamental knowledge, structure-property relationships and structure modification strategies for: Solubility, Permeability, Metabolic Stability, Pharmacokinetics, CYP Inhibition, CYP Induction, Plasma Protein Binding, Drug Metabolites, hERG, Pgp Efflux, Uptake Transporters, Prodrugs, Plasma and Solution Stability, Lipophilicity, pKa, Rule of 5, Blood-Brain Barrier, Formulation for Animal Dosing Studies, and Toxicity.
  • Assays for Each Property – Introduction to the leading property assays to assist you with informed decisions in applying assay data, selecting the right assay for your needs, and correlation to pharmacokinetics and toxicity.
  • Applying Property Data to Structure Modification – How structure modifications affect properties, structure modification strategies for each property from the med chem literature, and case studies from successful projects.
  • Individual and Group Exercises – Interpretation of data, selecting properties relevant to your specific question, selecting an appropriate assay to answer your questions, modifying structures to improve properties, frequently asked questions and answers.

Course Locations

Date

TBA

Check-in opens at 7:30 a.m. on the first day of the course.

Course runs from 8:30 a.m. to 5:00 p.m. each day.

Register Online Register Via Mail

Venue

TBA


Pricing
  Member Non-Member
Advanced $1,495 (ends ) $1,695 (ends )
Standard $1,895 $2,095

The course fee includes a course binder and a continental breakfast each day.

Five for Four! Register five people for one course, one person for five courses, or any combination in between and your fifth registration is free. Note: This discount is only available if you register by fax or mail and mention this discount. May not be combined with any other offer.

About the Instructors

  • Edward H. Kerns

    has 34 years in drug discovery and development focused on ADMET properties and pharmacokinetics. He is co-author of the book Drug-Like Properties: Concepts, Structure Design and Methods, and has written and lectured widely.

  • Li Di

    is Associate Research Fellow in Pharmacokinetics, Dynamics and Metabolism at Pfizer. She is involved with ADME property assessment, method development and consults with teams on property optimization.